Literature

Abstract

In this work, a series of 2-substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamide derivatives were developed as β-secretase (BACE-1) inhibitors. Supported by docking study, a small library of derivatives were designed, synthesized and biologically evaluated in vitro. In addition, the selected compounds were tested with affinity (KD) towards BACE-1, blood brain barrier (BBB) permeability and cytotoxicity. The studies revealed that the most potent analog 41 (IC50 = 4.6 μM) with high predicted BBB permeability and low cellular cytotoxicity, could serve as a good lead structure for further optimization.

DOI： 10.1016/j.ejmech.2017.06.020

2-Substituted-thio- N -(4-substituted-thiazol/1 H -imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies

European Journal of Medicinal Chemistry 2017.0

4-Oxo-1,4-dihydro-quinoline-3-carboxamides as BACE-1 inhibitors: Synthesis, biological evaluation and docking studies

European Journal of Medicinal Chemistry 2014.0

A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation

European Journal of Medicinal Chemistry 2012.0

Design, synthesis and evaluation of 2-amino-imidazol-4-one derivatives as potent β-site amyloid precursor protein cleaving enzyme 1 (BACE-1) inhibitors

Bioorganic & Medicinal Chemistry Letters 2019.0

Discovery of a Series of Efficient, Centrally Efficacious BACE1 Inhibitors through Structure-Based Drug Design

Journal of Medicinal Chemistry 2015.0

Design, synthesis and biological evaluation of tasiamide B derivatives as BACE1 inhibitors